TOPROL-XL

What it is

TOPROL-XL is a modified release tablet containing metoprolol succinate, available in strengths of 23.75 mg, 47.5 mg, 95 mg, and 190 mg. TOPROL-XL is recommended for once daily treatment and is preferably taken together with the morning meal. TOPROL-XL tablets should be swallowed with liquid and should not be chewed or crushed.

Approved indications

— Stable, chronic heart failure as an adjunct to other heart failure therapy.

Dosing overview

The dose of TOPROL-XL should be individually adjusted in patients with chronic heart failure stabilised on other heart failure treatment. Patients are recommended to be titrated from an initial dose of TOPROL-XL 23.75 mg (½ or 1 tablet daily for 2 weeks), then increased to TOPROL-XL 47.5 mg (1 tablet daily for 2 weeks), then TOPROL-XL 95 mg (1 tablet daily for 2 weeks), with progression to TOPROL-XL 190 mg or the highest tolerated dose. Patients with moderate to severe heart failure (NYHA III–IV) are recommended to start treatment with half a TOPROL-XL 23.75 mg tablet once daily for one week, then take a full TOPROL-XL 23.75 mg tablet once daily for the second week. During long-term treatment, the aim should be to reach TOPROL-XL 190 mg once daily or the highest tolerated dose. The patient should be carefully evaluated at each dose level with regard to tolerability.

Key safety warnings

Some patients may experience an initial, usually transient, worsening of the symptoms and signs of heart failure when starting treatment with TOPROL-XL, and if this occurs, the patient should be monitored very closely and the dose should be reduced if symptoms continue to worsen. TOPROL-XL should not be ceased abruptly due to the risk of rebound hypertension and tachycardia; if treatment is to be discontinued, it should be reduced gradually. If there is a need to discontinue treatment, this should be done gradually over at least two weeks with the dose reduced by half in each step, down to a final dose of half a 23.75 mg tablet, with the final dose taken for at least four days before discontinuation. TOPROL-XL should be used with caution in patients with diabetes mellitus, especially those receiving insulin or oral hypoglycaemic agents, as β-blockers affect glucose metabolism and may mask some important premonitory signs of acute hypoglycaemia, such as tachycardia. Where TOPROL-XL is prescribed for patients known to be suffering from asthma, an inhaled β₂-agonist should be administered, though the risk of TOPROL-XL interfering with β₂-receptors is less than with conventional tablet formulations of β₁-selective blockers.

Contraindications

TOPROL-XL is contraindicated in any patient with a history of airways obstruction or a tendency to bronchospasm. TOPROL-XL is also contraindicated in allergic disorders (including allergic rhinitis) which may suggest a predisposition to bronchospasm, right ventricular failure secondary to pulmonary hypertension, significant right ventricular hypertrophy, second and third degree atrioventricular block, shock (including cardiogenic and hypovolaemic shock), and unstable decompensated congestive heart failure (pulmonary oedema, hypoperfusion or hypotension). TOPROL-XL is contraindicated in continuous or intermittent inotropic therapy acting through β-receptor agonism, clinically relevant sinus bradycardia (less than 45–50 beats per minute), and non-compensated congestive heart failure. TOPROL-XL is contraindicated in sick-sinus syndrome (unless a permanent appropriately functioning pacemaker is in place), severe peripheral arterial circulatory disorders, suspected acute myocardial infarction with a heart rate of less than 45 beats per minute, a P–R interval of greater than 0.24 seconds or a systolic blood pressure of less than 100 mmHg and/or moderate to severe non-compensated heart failure, hypotension, and untreated phaeochromocytoma. TOPROL-XL is contraindicated in hypersensitivity to any component of TOPROL-XL and related derivatives.

Regulatory history

TOPROL-XL was first listed on the ARTG on 28 October 2003, with four strength variants registered (23.75 mg, 47.5 mg, 95 mg, and 190 mg).